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元宝枫树叶提取物:一种具有抗肿瘤活性的脂肪酸合酶天然抑制剂。

The extract of leaves of Acer truncatum Bunge: A natural inhibitor of fatty acid synthase with antitumor activity.

作者信息

Zhao Wen-Hua, Zhang Jin-Feng, Zhang Ying-Xia, Tian Wei-Xi

机构信息

Department of Chemical Biology, Capital University of Medical Sciences, Beijing 100069, China.

出版信息

J Enzyme Inhib Med Chem. 2006 Oct;21(5):589-96. doi: 10.1080/14756360600774579.

Abstract

Fatty acid synthase (FAS) has been identified as a potential antitumor target. The extract from the leaves of Acer truncatum Bunge (Extr) was prepared to assay its inhibitory activity against FAS, which was isolated from duck liver, and the correlated antitumor bioactivity. Its inhibition of FAS is composed of reversible fast-binding inhibition, IC50 = 0.7 microg/ml, and irreversible slow-binding inhibition following saturation kinetics with a dissociation constant of 0.68 microg/ml and a limiting rate constant of 0.0288 min(-1). The Extr exhibited different type of inhibitions against the three substrates in the FAS overall reaction. Compared with EGCG in inhibition constant and IC50 value, the Extr appeared to be a more efficient inhibitor, and exhibited a considerable inhibition against the growth of four kinds of cancer cells (patent application number 200510068054.2). It was infered that the inhibitory activity is likely attributable to the co-operative effect of the components.

摘要

脂肪酸合酶(FAS)已被确定为一个潜在的抗肿瘤靶点。制备了元宝枫叶提取物(Extr),以检测其对从鸭肝中分离出的FAS的抑制活性以及相关的抗肿瘤生物活性。其对FAS的抑制作用由可逆的快速结合抑制(IC50 = 0.7微克/毫升)和遵循饱和动力学的不可逆缓慢结合抑制组成,解离常数为0.68微克/毫升,极限速率常数为0.0288分钟-1。Extr对FAS总反应中的三种底物表现出不同类型的抑制作用。与表没食子儿茶素没食子酸酯(EGCG)的抑制常数和IC50值相比,Extr似乎是一种更有效的抑制剂,并且对四种癌细胞的生长表现出相当大的抑制作用(专利申请号200510068054.2)。据推测,这种抑制活性可能归因于各成分的协同作用。

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